SGLT2 Inhibitor

WAY-123783 is a potent, selective and orally active sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor producing activity after metabolism. WAY-123783 can increase the excretion of sugar in urine and at the same time lower the blood sugar level in db/db mice (ED₅₀ = 9.85 mg/kg). WAY-123783 can be used for the research of metabolic disease, such as diabetes.

Velagliflozin proline is an oral sodium-glucose cotransporter 2 (SGLT2) inhibitor with antidiabetic activity. Velagliflozin proline reduces renal glucose reabsorption and stimulates glycosuria, which lowers blood sugar and insulin concentrations.

SGLT1/2-IN-8 (compound 8) is a potent and orally active SGLT1/2 dual inhibitor with IC₅₀ values of 4 nM and 1 nM, respectively. SGLT1/2-IN-8 exhibits anti-hyperglycemic effects and can be utilized in relevant research.

YM-543 is a selective SGLT2 inhibitor that effectively reduces hyperglycemia in type 2 diabetic mice through increased urinary glucose excretion. YM-543 demonstrates potent inhibition of both mouse and human SGLT2 activities at nanomolar concentrations. YM-543, when administered orally, significantly improves glucose tolerance in diabetic models and sustains its effects for over 12 hours. YM-543, in combination with other antidiabetic agents like rosiglitazone or metformin, enhances the therapeutic effects on diabetic symptoms. YM-543 does not affect blood glucose levels in normal mice, indicating its specificity for diabetic conditions.

LX2761 is an orally active, dual SGLT1/SGLT2 inhibitor with IC₅₀ values of 2.2 nM and 2.7 nM against human SGLT1 and SGLT2, respectively. LX2761 locks human SGLT1 in an outward-open conformation and blocks its putative water permeation pathway. After oral administration, LX2761 is confined exclusively to the intestinal lumen, delays intestinal glucose absorption, regulates intestinal glucose metabolism, increases cecal glucose levels, reduces cecal pH, improves glycemic control and elevates plasma total GLP-1 levels. However, LX2761 induces diarrhea in a dose-dependent manner. LX2761 can be used in diabetes-related research.

SAR-7226 is a SGLT1 and SGLT2 dual inhibitor. SAR-7226 can be used for research of type 2 diabetes.

Pragliflozin-¹³C₆ (ASP1941-¹³C₆) is ¹³C labeled Ipragliflozin. Ipragliflozin (ASP1941) is an orally active and selective SGLT2 inhibitor with IC₅₀s of 7.38 and 1876 nM, 6.73 and 1166 nM, 5.64 and 1380 nM for human SGLT2 and SGLT1, rat SGLT2 and SGLT1, mouse SGLT2 and SGLT1, respectively. Antidiabetic agent.

Velagliflozin proline hydrate is the clinical form of Velagliflozin (HY-109018). Velagliflozin is an oral sodium-glucose cotransporter 2 (SGLT2) inhibitor with antidiabetic activity. Velagliflozin reduces renal glucose reabsorption and stimulates glycosuria, which lowers blood sugar and insulin concentrations.

Janagliflozin is orally active and highly selective sodium-glucose cotransporter 2 (SGLT2) inhibitor (IC₅₀=0.0058 μM for SGLT2 and 4.802 μM for SGLT1). Janagliflozin inhibits SGLT2 in the proximal renal tubules, reducing glucose reabsorption and promoting urinary glucose excretion (UGE) to lower blood glucose levels. Janagliflozin is promising for research of type 2 diabetes mellitus.

TA-1887 (JNJ-39933673) is a highly potent, selective and orally active SGLT2 inhibitor (IC₅₀: 1.4 nM) with antihyperglycemic effects. TA-1887 can be used in the research of diabetes.

SGLT2-IN-3 is a sodium-glucose co-transporter 2 (SGLT2) inhibitor. SGLT2-IN-3 can inhibit glucose uptake. SGLT2-IN-3 can be used for the research of metabolic disease, such as diabetes.

YM543 free base is a potent and orally active sodium-glucose cotransporter (SGLT) 2 inhibitor. YM543 free base reduces blood glucose levels. YM543 free base can be used in research of diabetes.

Trilobatin (Standard) is the analytical standard of Trilobatin. This product is intended for research and analytical applications. Trilobatin, a natural sweetener derived from?Lithocarpus polystachyus?Rehd, Trilobatin?is an HIV-1 entry inhibitor targeting the HIV-1 Gp41 envelope. Neuroprotective effects. Trilobatin is also a SGLT1/2 inhibitor that selectively induces the proliferation of human hepatoblastoma cells.

SGLT2-IN-5 (Compound 99) is an orally active SGLT2 inhibitor with IC₅₀ values for SGLT2, SGLT1, and DPP4 of 0.8, 23, and 58 nM respectively. SGLT2-IN-5 controls blood sugar levels in diabetic rat models and increases the levels of active GLP-1. SGLT2-IN-5 can be used for the study of type 2 diabetes.

Canagliflozin (Standard) is the analytical standard of Canagliflozin. This product is intended for research and analytical applications. Canagliflozin (JNJ 28431754) is a selective SGLT2 inhibitor with IC₅₀s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively.

Ipragliflozin (Standard) is the analytical standard of Ipragliflozin. This product is intended for research and analytical applications. Ipragliflozin (ASP1941) is an orally active and selective SGLT2 inhibitor with IC₅₀s of 7.38 and 1876 nM, 6.73 and 1166 nM, 5.64 and 1380 nM for human SGLT2 and SGLT1, rat SGLT2 and SGLT1, mouse SGLT2 and SGLT1, respectively. Antidiabetic agent.

SGLT2-IN-6 (Compound 101) is an orally active SGLT2 inhibitor with IC₅₀ values for SGLT2, SGLT1, and DPP4 of 0.8, 6.7, and 72 nM respectively. SGLT2-IN-6 controls blood sugar levels in diabetic rat models and increases the levels of active GLP-1. SGLT2-IN-6 can be used for the study of type 2 diabetes.

Bexagliflozin diproline (EGT1442 diproline; EGT0001442 diproline; THR-1442 diproline) is an orally active and selective SGLT2 inhibitor with IC₅₀ values of 0.002 μM and 5.6 μM for SGLT2 and SGLT1, respectively. Bexagliflozin diproline selectively inhibits SGLT2-mediated sodium-dependent glucose uptake. Bexagliflozin diproline induces saturable urinary glucose excretion in normal rats and dogs. Bexagliflozin diproline reduces blood glucose and HbA_1c levels in db/db mice without affecting body mass or insulin level. Bexagliflozin diproline can be used for the research of type 2 diabetes mellitus, hypertensive stroke.

Phlorizin (Floridzin) (Standard) is the analytical standard of Phlorizin. This product is intended for research and analytical applications. Phlorizin is an orally active non-selective sodium-glucose cotransporter (SGLT) inhibitor, with an IC₅₀ of 0.04 μM and a K_i of 39 nM against hSGLT2, and an IC₅₀ of 0.17 μM and a K_i of 0.31 μM against hSGLT1. Phlorizin promotes GLUT4 translocation, inhibits gluconeogenesis and promotes glycogen synthesis by activating the PI3K/Akt/mTOR pathway. Phlorizin reduces DNA damage and apoptosis (apoptosis) by inhibiting the NF-κB inflammatory pathway. Phlorizin induces apoptosis via activating the Caspase pathway by antagonizing the JAK/STAT3 and PCK pathways. Phlorizin also exhibits antibacterial, anti-inflammatory and neuroprotective activities.

TP0438836 (compound 30b) is a SGLT1 inhibitor, with IC₅₀ values ​​of 28 nM and 7 nM for hSGLT1 and hSGLT2, respectively. TP0438836 can be used in diabetes research.